US6642219B1ExpiredUtility

Progestogen-antiprogestogen regimens

Assignee: AKZO NOBEL NVPriority: Nov 14, 1997Filed: Nov 11, 1998Granted: Nov 4, 2003
Est. expiryNov 14, 2017(expired)· nominal 20-yr term from priority
A61P 15/00A61P 15/18A61K 31/57A61K 31/565
42
PatentIndex Score
3
Cited by
28
References
5
Claims

Abstract

An estrogen-free contraceptive is provided which does not have the bleeding-related drawbacks of conventional progestogen-only pills. Thus the invention is a contraceptive kit comprising a combined means for the simultaneous daily administration of a progestogen as the sole contraceptively effective ingredient and an anti-progestogen. Said combined means preferably is in the form of tablets having a normal contraceptive dose of the progestogen and low dose of the anti-progestogen.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
       1. A method of treating intermenstrual bleeding in a female, the bleeding induced by administration to the female of a progestogen-only contraceptive regimen on a continuous daily basis, wherein the improvement comprises: 
       co-administering, on the continuous daily basis for at least 28 consecutive days with the progestogen, an anti-progestogen at a daily dose equivalent, in anti-progestational activity, to a dose of (11β,17β)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl) estra-4,9-diene-3-one of from 0.05 mg to 5 mg to reduce bleeding in the female.  
     
     
       2. The method according to clam  1 , wherein the daily dose of anti-progestogen is equivalent, in anti-progestational activity, to a dose of (11β,17β)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-diene-3-one of from 0.1 to 2 mg. 
     
     
       3. A method of contraception that inhibits ovulation in a female without increasing the frequency of intermenstrual bleeding, said method comprising: 
       simultaneously administering to a female, every day for a period of at least 28 days, without a progestogen and anti-progestogen free day:  
       progestogen in a daily dosage amount sufficient to inhibit ovulation in the female, and  
       anti-progestogen in a daily dosage amount corresponding in anti-progestational activity to from 0.05 mg to 5 mg of (11β,17β)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-diene-3-one thus inhibiting ovulation in the female without increasing the frequency of intermenstrual bleeding.  
     
     
       4. The method according to  claim 3 , wherein the daily dose of anti-progestogen is equivalent to a dose of (11β,17β)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-diene-3-one of from 0,1 to 2 mg. 
     
     
       5. The method according to  claim 3 , wherein the progestogen is desogestrel, gestodene, or (17α)-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20yh-3-one and the anti-progestogen is (11β,17β)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-diene-3-one, (6α,11β,17β)-11-(4-dimethylaminophenyl)-6-methyl-4′,5′-dihyrospiro-[estra-4,9-diene-17,2′-(3′H)-furan]-3-one or (11β,17α)-11-(4-acetylphenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one.

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